Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM0X36Y)

Drug Name

Ritanserin Drug Info

Synonyms

ritanserin; 87051-43-2; Tiserton; Ritanserine; Ritanserinum; Ritanserina; R-55667; Ritanserinum [Latin]; Ritanserine [French]; Ritanserina [Spanish]; UNII-145TFV465S; C27H25F2N3OS; R 55,667; 6-(2-(4-(bis(4-fluorophenyl)methylene)piperidin-1-yl)ethyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one; MLS000069360; CHEMBL267777; 6-(2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl)-7-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one; N,N-dialkyl-dipeptidylamines

Indication

Disease Entry	ICD 11	Status	REF
Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[1]

Cross-matching ID

PubChem CID: 5074
ChEBI ID: CHEBI:64195
CAS Number: CAS 87051-43-2
TTD Drug ID: DM0X36Y

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 2 receptor (5HT2R)	TTYSN63	NOUNIPROTAC	Antagonist	[2]
5-HT 2A receptor (HTR2A)	TTJQOD7	5HT2A_HUMAN	Antagonist	[2]
5-HT 2B receptor (HTR2B)	TT0K1SC	5HT2B_HUMAN	Antagonist	[3]
5-HT 2C receptor (HTR2C)	TTWJBZ5	5HT2C_HUMAN	Antagonist	[2]
5-HT receptor (5HTR)	TT85JO3	NOUNIPROTAC	Antagonist	[4]
Voltage-gated calcium channel alpha Cav2.2 (CACNA1B)	TT4FDG6	CAC1B_HUMAN	Blocker	[5]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
5-HT 2C receptor (HTR2C)	DTT	HTR2C	4.233	3.329	3.843	3.888
5-HT 2A receptor (HTR2A)	DTT	HTR2A	4.84	4.904	4.652	4.129
Voltage-gated calcium channel alpha Cav2.2 (CACNA1B)	DTT	CACNA1B	4.087	2.433	1.632	3.392
5-HT 2B receptor (HTR2B)	DTT	HTR2B	0.485	3.536	0.379	4.667

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Anxiety disorder

ICD Disease Classification

6B00-6B0Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
5-HT 2A receptor (HTR2A)	DTT	HTR2A	7.61E-01	-0.65	-0.54
Voltage-gated calcium channel alpha Cav2.2 (CACNA1B)	DTT	CACNA1B	9.07E-01	7.11E-03	0.06

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 97).
2	Characterization of contractile 5-hydroxytryptamine receptor subtypes in the in situ autoperfused kidney in the anaesthetized rat. Eur J Pharmacol. 2008 Sep 11;592(1-3):133-7.
3	p-Chloroamphetamine, a serotonin-releasing drug, elicited in rats a hyperglycemia mediated by the 5-HT1A and 5-HT2B/2C receptors. Eur J Pharmacol. 1998 Oct 23;359(2-3):185-90.
4	Combined treatment of portal hypertension with ritanserin and propranolol in conscious and unrestrained cirrhotic rats. Hepatology. 1992 May;15(5):878-82.
5	N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Mar 22;9(6):907-12.